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G protein-coupled receptors (GPCRs) are heptahelical transmembrane
receptors that convert extra-cellular stimuli into intra-cellular
signaling, and ultimately into biological responses. Since GPCRs
are natural targets for approximately 40% of all modern medicines,
it is not surprising that they have been the subject of intense
research. Notwithstanding the amount of data generated over the
years, discovering ligands of these receptors with optimal
therapeutic properties is not straightforward and has certainly
been hampered for years by the lack of high-resolution structural
information about these receptors. Luckily, there has been a steady
increase of high-resolution crystal structures of these receptors
since 2007, and this information, integrated with dynamic
inferences from computational and experimental methods, holds great
potential for the discovery of new, improved drugs. This book,
which provides, for the first time, state-of-the-art views on
modeling and simulation of GPCRs, is divided into 4 parts. In the
first part, the impact of currently available GPCR crystal
structures on structural modeling is discussed extensively as are
critical insights from simulations in the second part of the book.
The third part reports recent progress in rational ligand discovery
and mathematical modeling, whereas the fourth part provides an
overview of bioinformatics tools and resources that are available
for GPCRs.
G protein-coupled receptors (GPCRs) are heptahelical transmembrane
receptors that convert extra-cellular stimuli into intra-cellular
signaling, and ultimately into biological responses. Since GPCRs
are natural targets for approximately 40% of all modern medicines,
it is not surprising that they have been the subject of intense
research. Notwithstanding the amount of data generated over the
years, discovering ligands of these receptors with optimal
therapeutic properties is not straightforward and has certainly
been hampered for years by the lack of high-resolution structural
information about these receptors. Luckily, there has been a steady
increase of high-resolution crystal structures of these receptors
since 2007, and this information, integrated with dynamic
inferences from computational and experimental methods, holds great
potential for the discovery of new, improved drugs. This book,
which provides, for the first time, state-of-the-art views on
modeling and simulation of GPCRs, is divided into 4 parts. In the
first part, the impact of currently available GPCR crystal
structures on structural modeling is discussed extensively as are
critical insights from simulations in the second part of the book.
The third part reports recent progress in rational ligand discovery
and mathematical modeling, whereas the fourth part provides an
overview of bioinformatics tools and resources that are available
for GPCRs.
This detailed volume provides an overview of recent techniques
employed in the field of G protein-coupled receptors (GPCRs) to
screen for new drugs and to derive information about their receptor
structure, dynamics, and function for the purpose of developing
improved therapeutics. Owing to remarkable recent advances in the
structural, biophysical and biochemical analyses of these
receptors, as well as a growing body of evidence hinting at the
possible relevance of allosteric modulators, biased agonists and
oligomer-selective ligands as improved therapeutic agents, drug
discovery for GPCRs has recently taken a completely new direction.
For this book, expert contributors have shared their protocols and
views on the impact of these methodologies on modern drug
discovery. Written for the highly successful Methods in Molecular
Biology series, chapters include introductions to their respective
topics, lists of the necessary materials and reagents,
step-by-step, readily reproducible laboratory protocols and tips on
troubleshooting and avoiding known pitfalls. Practical and fully
updated, G Protein-Coupled Receptors in Drug Discovery: Methods and
Protocols, Second Edition serves as an ideal guide for a diverse
audience from structural and molecular biologists to
pharmacologists and drug designers who wish to explore this
extensive class of key drug targets.
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